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Stimulants of the Future

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I wouldn't count noradrenaline out of the equation to produce a good stimulant compound. As long as the compound is lipophilic enough to primarily accumulate in the brain, NET substrates can release central noradrenaline, as well as dopamine in the frontal cortex via the NET (there are more NETs than DATs presynaptically in the prefrontral cortex, so some dopamine gets sucked up by adrenergic neurons). Since amphetamine (both d-amph and dl-amph) has equivalent affinity/efficacy at both the DAT and the NET, it has some decent cognition enhancing effects. d-Methamphetamine does have a greater affinity for dopamine transporters and while it is a more potent stimulant, it is also more hedonic (hence, addictive) with a weaker pro-cognitive effect and is significantly more toxic than amphetamine itself. Noradrenaline can be a good thing, as long as it's not peripherally creepy-crawly and all annoyingly hot and bothered--of course, some dopaminergic activity is essential, otherwise the whole thing just gets disgusting, like (-)-ephedrine, phentermine or atomoxetine.
 
Forgive me, if necessary, for not having just read this entire 35 page thread, but in the spirit of "not counting noradrenaline out," what about the six
(3,4-MD)-(50:50 R/S)-beta-methoxy(meth,eth)amphetamines?

2C-beta-MeO-MDA is active, according to PiHKAL (in which it has its own entry), and none of the above 6 compounds would be particularly hard to make, especially (R, S, or 50:50 R/S)-beta-MeO-methamphetamine.
 
What about the possibility of indolic stimulants? I mean, indolic compounds have shown a wide range of biological effects, and yohimbine is an indole and a fairly powerful stimulant. Although a fair amount of indolic compounds are psychedelic, you have things like the harmal alkaloids and ibogaine, which do wierd things fairly different from the more typical indolic psychedelics. And you also have stuff like AMT, which has an almost MDMA like effect (the closest thing I've come by to it in several regards) albeit a very psychedelic one.

Is the likelihood of powerful indolic stimulants possible in the same way that phenethylamines can run the gamut from balls-trippy psychedelic compounds, thru sort of semi-psychedelic euphoriants like MDA, to very plainly stimulating ones, or is the fact that there are relatively few if any straight up indolic stimulants with amphetamine-like effects indicative of the unlikeliness of it being possible? Could anyone with a better knowledge of neuropharmacology and organic chemistry than I have enlighten me? I'm sure this territory has to have been charted a little bit at least.
 
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Indoles are wicked. Just look at all the recent problems with JWH-018, for example.

Yeah, I know that there's got to be a Yin for every Yang and all that, but Lord, take a whiff.
 
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I am far from a chemist myself, so I cant comment on chemically altering stimulants to make more effective/euphoric. Just throught it would be useful to mention here that I did read up that a new drug is being passed by the FDA in the US, which is a transdermal extended release patch of the drug, mehtylphenidate. Supposedly this new patch will last 9 hours and will provide superior drug deliverence of the ritalin (methylphenidate) into the system. That should be interesting to see where it is scheduled and what the abuse potential of the new transdermal system is.
 
^Most of the time, addictiveness is (party) determined by steepness of the concentration of the drug in the brain, aka the "rush". (That's a big reason why people IV their stuff).

Transdermal is a pretty slow delivery mechanism afaik, so I guess it doesn't promote addictiveness / abuse potential.
 
^ correct, unless load is really high, such as if you use a whole bunch of patches at once...it can be abused, but has somewhat less potential

if you cover yourself in patches though, well...=D

i assume for now it is considered as the same sched regardless of format

gotta love Xyrem is a CIII and GHB is a CI and CI designates there is NO medicinal use whatsoever

they can;t even keep blatant hypocrisy out of their legislation...pathetic...
 
BilZ0r said:
Stimulants I think are one thing that people could hold out some hope for a new, plant derived drug. The monoamine transporters are so promiscuous, it seems all you need is a benzene and a nitrogen somewhere... and your in.
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I think that classes of stimulants basically discovered so far are those that affect DA and NE (the amphetamine type) and DA, NE and 5HT (the cocaine type). But further differentiation may come into play with those that affect the DAT vs those that affect the VMAT-2, and they may already be available.

The other possibility will (IMHO) be stimulants that affect orexin (modafinil being one of the first of its type, with a very weak orexin interaction.)

I am convinced that aminorex and 4-methyl-aminorex work through some alternative method, although my evidence is anecdotal.

MobiusDick
 
I am convinced that aminorex and 4-methyl-aminorex work through some alternative method, although my evidence is anecdotal.
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If by 'work through' you mean they have some other minor interaction: possibly. We have numbers showing that they're potent DARIs though. Or were they primarily releasers? oh well.
 
Hammilton said:
If by 'work through' you mean they have some other minor interaction: possibly. We have numbers showing that they're potent DARIs though. Or were they primarily releasers? oh well.
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indeed they are notably dopaminergic in their mode of action
 
5-(2-Aminopropyl)-indole (the "5" AMT analog) is an active, long lasting stimulant at 20mg,per THIKAL,you can read it up under AMT there,the other isomers are also discussed as is the "Phentermine" analog.


Nibiru said:
What about the possibility of indolic stimulants? I mean, indolic compounds have shown a wide range of biological effects, and yohimbine is an indole and a fairly powerful stimulant. Although a fair amount of indolic compounds are psychedelic, you have things like the harmal alkaloids and ibogaine, which do wierd things fairly different from the more typical indolic psychedelics. And you also have stuff like AMT, which has an almost MDMA like effect (the closest thing I've come by to it in several regards) albeit a very psychedelic one.

Is the likelihood of powerful indolic stimulants possible in the same way that phenethylamines can run the gamut from balls-trippy psychedelic compounds, thru sort of semi-psychedelic euphoriants like MDA, to very plainly stimulating ones, or is the fact that there are relatively few if any straight up indolic stimulants with amphetamine-like effects indicative of the unlikeliness of it being possible? Could anyone with a better knowledge of neuropharmacology and organic chemistry than I have enlighten me? I'm sure this territory has to have been charted a little bit at least.
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^^ I really like the look of this molecule. It is an interesting variation on the traditional 3,4-substituted amphetamines. I vaguely recall discussing it on bluelight years and years ago, thinking that it might be a good non-neurotoxic MDA analogue, lacking the problem of conversion to pro-oxidant metabolites via the 3,4-dihydroxyamphetamine intermediate.

The only conceivable problem with it might be activity the 5-HT2B receptor...which could only be revealed by an in vitro receptor binding/efficacy study.
 
Ring aminated phenethylamine like stimulants tend to be even more toxic... if metabolism breaks the ring open you'll end up with an aniline.
 
Not an indole, but somewhat related is mazindol with it's impressive NE reuptake inhibition.
 
nuke said:
Ring aminated phenethylamine like stimulants tend to be even more toxic... if metabolism breaks the ring open you'll end up with an aniline.
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Well if the indole ring could be broken up by metabolism, wouldn't that also make all the tryptamines toxic?

Anyway, what about the benzofuran and benzothiophene analogues of this chemical...
 
Mazindol is just plain strange.

It's not rewarding, but it definitely has sympathomimetic properties, making it pretty much a stimulant. Modafanil isn't very rewarding either, and neither is yohimbine, arguably, but they are definitely stimulating.
 
i would consider all those stimulants as that is a primary effect even if overall they are not classical in nature

few, but some, i believe can get a nice effect off Maz...nothing stunning, but as with Yohimbine it is very user specific as to a good, bad, or ugly effect

obviously modafinil is a stimulant and rarely has any negative effects, though indeed it is not usually recreational for anyone, but can aid functional capacity greatly
 
Mazindol is definitely a stimulant--it will keep you awake. It is somewhat interesting in the fact that it is rather translucent: it doesn't feel good, but it also doesn't feel particularly bad. Yohimbine, on the other hand, is simply disgustipating in every way.
 
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